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Selective USP7 inhibition elicits cancer cell killing through a p53-dependent mechanism.
Schauer NJ, Liu X, Magin RS, Doherty LM, Chan WC, Ficarro SB, Hu W, Roberts RM, Iacob RE, Stolte B, Giacomelli AO, Perera S, McKay K, Boswell SA, Weisberg EL, Ray A, Chauhan D, Dhe-Paganon S, Anderson KC, Griffin JD, Li J, Hahn WC, Sorger PK, Engen JR, Stegmaier K, Marto JA, Buhrlage SJ. Schauer NJ, et al. Sci Rep. 2020 Mar 24;10(1):5324. doi: 10.1038/s41598-020-62076-x. Sci Rep. 2020. PMID: 32210275 Free PMC article.
Inhibition of USP10 induces degradation of oncogenic FLT3.
Weisberg EL, Schauer NJ, Yang J, Lamberto I, Doherty L, Bhatt S, Nonami A, Meng C, Letai A, Wright R, Tiv H, Gokhale PC, Ritorto MS, De Cesare V, Trost M, Christodoulou A, Christie A, Weinstock DM, Adamia S, Stone R, Chauhan D, Anderson KC, Seo HS, Dhe-Paganon S, Sattler M, Gray NS, Griffin JD, Buhrlage SJ. Weisberg EL, et al. Nat Chem Biol. 2017 Dec;13(12):1207-1215. doi: 10.1038/nchembio.2486. Epub 2017 Oct 2. Nat Chem Biol. 2017. PMID: 28967922 Free PMC article.
Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors.
Sivakumaren SC, Shim H, Zhang T, Ferguson FM, Lundquist MR, Browne CM, Seo HS, Paddock MN, Manz TD, Jiang B, Hao MF, Krishnan P, Wang DG, Yang TJ, Kwiatkowski NP, Ficarro SB, Cunningham JM, Marto JA, Dhe-Paganon S, Cantley LC, Gray NS. Sivakumaren SC, et al. Cell Chem Biol. 2020 May 21;27(5):525-537.e6. doi: 10.1016/j.chembiol.2020.02.003. Epub 2020 Mar 3. Cell Chem Biol. 2020. PMID: 32130941 Free PMC article.
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Manz TD, Sivakumaren SC, Yasgar A, Hall MD, Davis MI, Seo HS, Card JD, Ficarro SB, Shim H, Marto JA, Dhe-Paganon S, Sasaki AT, Boxer MB, Simeonov A, Cantley LC, Shen M, Zhang T, Ferguson FM, Gray NS. Manz TD, et al. ACS Med Chem Lett. 2019 Nov 3;11(3):346-352. doi: 10.1021/acsmedchemlett.9b00402. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184968 Free PMC article.
Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Manz TD, Sivakumaren SC, Ferguson FM, Zhang T, Yasgar A, Seo HS, Ficarro SB, Card JD, Shim H, Miduturu CV, Simeonov A, Shen M, Marto JA, Dhe-Paganon S, Hall MD, Cantley LC, Gray NS. Manz TD, et al. J Med Chem. 2020 May 14;63(9):4880-4895. doi: 10.1021/acs.jmedchem.0c00227. Epub 2020 Apr 27. J Med Chem. 2020. PMID: 32298120 Free PMC article.
Identification of a Structural Determinant for Selective Targeting of HDMX.
Ben-Nun Y, Seo HS, Harvey EP, Hauseman ZJ, Wales TE, Newman CE, Cathcart AM, Engen JR, Dhe-Paganon S, Walensky LD. Ben-Nun Y, et al. Structure. 2020 Jul 7;28(7):847-857.e5. doi: 10.1016/j.str.2020.04.011. Epub 2020 Apr 30. Structure. 2020. PMID: 32359398 Free PMC article.
Identification of a Covalent Molecular Inhibitor of Anti-apoptotic BFL-1 by Disulfide Tethering.
Harvey EP, Hauseman ZJ, Cohen DT, Rettenmaier TJ, Lee S, Huhn AJ, Wales TE, Seo HS, Luccarelli J, Newman CE, Guerra RM, Bird GH, Dhe-Paganon S, Engen JR, Wells JA, Walensky LD. Harvey EP, et al. Cell Chem Biol. 2020 Jun 18;27(6):647-656.e6. doi: 10.1016/j.chembiol.2020.04.004. Epub 2020 May 14. Cell Chem Biol. 2020. PMID: 32413285 Free PMC article.
132 results